WO2014140784A3 - Buprenorphine analogs - Google Patents

Buprenorphine analogs Download PDF

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Publication number
WO2014140784A3
WO2014140784A3 PCT/IB2014/000394 IB2014000394W WO2014140784A3 WO 2014140784 A3 WO2014140784 A3 WO 2014140784A3 IB 2014000394 W IB2014000394 W IB 2014000394W WO 2014140784 A3 WO2014140784 A3 WO 2014140784A3
Authority
WO
WIPO (PCT)
Prior art keywords
formula
buprenorphine
compounds
buprenorphine analogs
analogs
Prior art date
Application number
PCT/IB2014/000394
Other languages
French (fr)
Other versions
WO2014140784A2 (en
Inventor
Richard R. Goehring
Laykea Tafesse
Jiangchao Yao
Original Assignee
Purdue Pharma L.P.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Purdue Pharma L.P. filed Critical Purdue Pharma L.P.
Priority to CA2905678A priority Critical patent/CA2905678A1/en
Priority to JP2015562364A priority patent/JP6203871B2/en
Priority to EP14713577.6A priority patent/EP2970321B1/en
Publication of WO2014140784A2 publication Critical patent/WO2014140784A2/en
Publication of WO2014140784A3 publication Critical patent/WO2014140784A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/02—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10—Laxatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/09—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems
    • C07D489/10—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14
    • C07D489/12—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14 the bridge containing only two carbon atoms

Abstract

The present invention is directed to Buprenorphine Analog compounds of Formula (I), (II) or (III) and including various stereoisomers (such as Formula (IA) shown below), wherein R1, R3a, R3b, R16, R15, G, Q, X, and Z are as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.
PCT/IB2014/000394 2013-03-15 2014-03-14 Buprenorphine analogs WO2014140784A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
CA2905678A CA2905678A1 (en) 2013-03-15 2014-03-14 Buprenorphine analogs
JP2015562364A JP6203871B2 (en) 2013-03-15 2014-03-14 Buprenorphine analogue
EP14713577.6A EP2970321B1 (en) 2013-03-15 2014-03-14 Buprenorphine analogs

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361786997P 2013-03-15 2013-03-15
US61/786,997 2013-03-15

Publications (2)

Publication Number Publication Date
WO2014140784A2 WO2014140784A2 (en) 2014-09-18
WO2014140784A3 true WO2014140784A3 (en) 2015-03-12

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2014/000394 WO2014140784A2 (en) 2013-03-15 2014-03-14 Buprenorphine analogs

Country Status (6)

Country Link
US (2) US8969358B2 (en)
EP (1) EP2970321B1 (en)
JP (1) JP6203871B2 (en)
CA (1) CA2905678A1 (en)
TW (1) TW201446769A (en)
WO (1) WO2014140784A2 (en)

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WO2014087226A1 (en) 2012-12-07 2014-06-12 Purdue Pharma L.P. Buprenorphine analogs as opiod receptor modulators
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US8980906B2 (en) 2012-12-14 2015-03-17 Purdue Pharma L.P. Pyridonemorphinan analogs and biological activity on opioid receptors
EP2951160B1 (en) 2013-01-31 2019-04-24 Purdue Pharma LP Benzomorphan analogs and the use thereof
US8969358B2 (en) * 2013-03-15 2015-03-03 Purdue Pharma L.P. Buprenorphine analogs
JP6353543B2 (en) 2013-12-26 2018-07-04 パーデュー、ファーマ、リミテッド、パートナーシップ Ring contraction morphinan and use thereof
US9994571B2 (en) 2013-12-26 2018-06-12 Purdue Pharma L.P. 10-substituted morphinan hydantoins
US9988392B2 (en) 2013-12-26 2018-06-05 Purdue Pharma L.P. 7-beta-alkyl analogs of orvinols
US9340542B2 (en) 2013-12-26 2016-05-17 Purdue Pharma L.P. Propellane-based compounds and the use thereof
WO2015097545A1 (en) 2013-12-26 2015-07-02 Purdue Pharma L.P. Opioid receptor modulating oxabicyclo[2.2.2]octane morphinans
US10550088B2 (en) 2013-12-27 2020-02-04 Purdue Pharma L.P. 6-substituted and 7-substituted morphinan analogs and the use thereof
EP3139921A4 (en) 2014-05-06 2018-02-14 Purdue Pharma L.P. Benzomorphan analogs and use thereof
CA2950567A1 (en) 2014-05-27 2015-12-03 Purdue Pharma L.P. Spirocyclic morphinans and use thereof
EP3154971A4 (en) 2014-06-13 2017-11-01 Purdue Pharma L.P. Heterocyclic morphinan derivatives and use thereof
JP6360915B2 (en) 2014-06-13 2018-07-18 パーデュー、ファーマ、リミテッド、パートナーシップ Azamorphinan derivatives and uses thereof
MA41125A (en) 2014-12-05 2017-10-10 Purdue Pharma Lp 6.7-CYCLOMORPHINANE DERIVATIVES AND THEIR USE
EP3458061B1 (en) * 2016-05-19 2023-01-18 Virginia Commonwealth University Potent and selective mu opioid receptor modulators
WO2018125716A1 (en) 2017-01-02 2018-07-05 Purdue Pharma L.P. Morphinan derivatives and use thereof

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Also Published As

Publication number Publication date
US20150203504A1 (en) 2015-07-23
EP2970321B1 (en) 2018-06-27
JP2016514122A (en) 2016-05-19
US8969358B2 (en) 2015-03-03
US20140275117A1 (en) 2014-09-18
EP2970321A2 (en) 2016-01-20
CA2905678A1 (en) 2014-09-18
WO2014140784A2 (en) 2014-09-18
US9382260B2 (en) 2016-07-05
JP6203871B2 (en) 2017-09-27
TW201446769A (en) 2014-12-16

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